Syntheses and biological studies of novel spiropiperazinyl oxazolidinone antibacterial agents using a spirocyclic diene derived acylnitroso Diels鈭扐lder reaction

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• 作者：Cheng Ji^a ; Weimin Lin^a ; Garrett C. Moraski^a ; Jane A. Thanassi^b ; Michael J. Pucci^b ; Scott G. Franzblau^c ; Ute Mö ; llmann^d ; Marvin J. Miller^a ; ^{mmiller1@nd.edu}
• 关键词：Oxazolidinone ; Antibiotics ; Nitroso Diels&minus ; Alder reaction ; Spirocyclic diene ; MRSA
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2012
• 期刊代码：9_09680896
• 类别：ch
• 出版时间：1 June, 2012
• 卷：20
• 期：11
• 页码：3422-3428
• 文件大小：438 K

摘要

Several novel oxazolidinone antibiotics with a spiropiperazinyl substituent at the 4鈥?position of the phenyl ring were synthesized through nitroso Diels-Alder chemistry and the in vitro antibacterial activities were evaluated against various Gram-positive bacteria (Bacillus subtilis, Staphylococcus aureus, Enterococcus faecalis), Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa) and mycobacteria (Mycobacterium vaccae, Mycobacterium tuberculosis). Analogs (8a and 12) were active against selected drug resistant microbes, like methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE) and had no mammalian toxicity in a Hep-2 cellular assay (CC₅₀ >100 渭M).